ANTICONVULSANT ACTIVITY OF ISONICOTINIC ACID HYDRAZONE DERIVATIVES USING MES, scPTZ AND ROTOROD NEUROTOXICITY MODELS

R Sinha, UVS Singh, RL Khosa, J Jain

Abstract


Introduction: Epilepsy is a chronic neurological disorder, involving group of nerve cells, or neurons, in the brain. Many classes of antiepileptic drugs are being prescribed and used by the stake holders but most of them are associated with serious side effects and toxicity. There is a strong need of new antiepileptic molecules with less side effects and toxicity. Objective: A series of aryl acid hydrazones of Isonicotinic acid hydrazide (RINH1 -RINH14) were synthesized and evaluated for Anticonvulsant activity. Material and Method: Compounds (RINH1 -RINH14) were synthesized by refluxing Isonicotinic acid hydrazide with different substituted benzaldehydes/ substituted acetophenones in absolute ethanol. Melting points of all synthesized compounds were monitored by open glass-capillary tube method on Digital Melting point apparatus and are uncorrected. The synthesized compounds were tested for anticonvulsant potential using MES and scPTZ whereas neurotoxicity was determined using Rotarod model. Result and Discussion: At 100mg/kg compound RINH10 have shown 29% protection at both 0.5hr and 4.0 time interval .At 300mg/kg and 0.5 hr, compounds RINH4 and RINH10 showed 100% and 50 % protection respectively. Compounds RINH4 and RINH10 have better anti MES activity proving that halogens have prominent contribution in Anticonvulsant activity. In scPTZ screen, all synthesized Acid hydrazone (RINH1- RINH14 ) did not show any protection at 30, 100,300 mg/kg , at 0.5 hr and 4.0 hr duration .In rotorod test i.e neurotoxicity screen, compound RINH5, RINH6 , RINH10 have shown toxicity. Conclusion: The synthesized new molecules were proved to be having anticonvulsant activity with less signs of neurotoxicity.

Keywords


Aryl acid Hydrazone,Anticonvulsant Activity,Isonicotinic acid hydrazone

Full Text:

PDF


DOI: https://doi.org/10.31069/japsr.v1i01.13058

Refbacks

  • There are currently no refbacks.